- 2,3-Dihalo- and 2,3,6,7-Tetrahaloanthracenes by Vollhardt Trimerization
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We efficiently synthesized otherwise difficult to obtain 2,3- and 2,3,6,7-halogenated anthracenes with diverse east/west substituents. Key steps involve the (i) Vollhardt cyclization of bis(propargyl)benzenes with bis(trimethylsilyl)acetylene, (ii) halo-desilylation introducing chlorine, bromine, or iodine substituents, and (iii) dehydrogenation. Pd catalysis allows selective functionalization at the anthracenes' east/west positions. A tetrahydropentacene is synthesized and derivatized via the same strategy, employing tetrapropargylbenzene.
- Hoffmann, Hendrik,Mukanov, Diana,Ganschow, Michael,Rominger, Frank,Freudenberg, Jan,Bunz, Uwe H. F.
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- IDO/TDO Inhibitor
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A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R1 and R2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R1 and R2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R4 represents, for example, —C(═NH)—HN2, and R6 represents, for example, a substituted or unsubstituted aryl group].
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Paragraph 0334; 0337; 0338; 0515-0517
(2020/08/19)
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- ALPHA-CINNAMIDE COMPOUNDS AND COMPOSITIONS AS HDAC8 INHIBITORS
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The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
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- GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
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- Substituted 5,6,11,12-tetradehydrodibenzo[ a, e ]cyclooctenes: Syntheses, properties, and DFT studies of substituted sondheimer-wong diynes
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Highly strained cyclic acetylenes 5,6,11,12-tetradehydrodibenzo[a,e]cyclooctenes (Sondheimer-Wong diynes) having various substituents on their benzene rings were synthesized successfully by one-pot treatment of the corresponding formyl sulfones with diethyl chlorophosphate/lithium hexamethyldisilazide (LiHMDS) and then lithium diisopropylamide (LDA). When mixtures of two types of formyl sulfones bearing different substituents were subjected to this protocol, the unsymmetrically substituted Sondheimer-Wong diynes could be synthesized in a stepwise manner by isolation of the heterocoupled vinyl sulfone intermediates followed by their treatment with LDA. The UV-vis absorption spectra and cyclic voltammograms of the substituted Sondheimer-Wong diynes were recorded. The electronic effect of substituents on the diynes was investigated in their click reactions and nucleophilic and electrophilic additions.
- Xu, Feng,Peng, Lifen,Shinohara, Kenta,Morita, Takamoto,Yoshida, Suguru,Hosoya, Takamitsu,Orita, Akihiro,Otera, Junzo
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p. 11592 - 11608
(2015/01/09)
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- SUBSTITUTED BENZOYLAMINO-INDAN-2-CARBOXYLIC ACIDS AND RELATED COMPOUNDS
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The present invention relates to A compound of the formula Ia wherein in any of its stereoisomers forms or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof, wherein the substituents are as described herein. The inventive compounds have CXCR5 inhibitory activity are particularly useful in treating or preventing various inflammatory diseases, such as rheumatoid arthritis, multiple sclerosis, lupus, Crohn's Disease, associated with the modulation of the human CXCR5 receptor.
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- MDR reversal agents
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Compounds of the general formula: STR1 wherein R1, R2, R3, R4 and R5 are herein described, A is a straight or branched (C2 -C12)alkyl or a phenyl moiety and B is a moiety of the formula: STR2 The compounds are effective in potentiating the activity of chemotherapeutic anti-cancer agents by increasing the sensitivity of multi-drug resistant cells to such chemotherapeutic agents.
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- Novel Substituted Poly(benzothiophenes); Controlling the n- and p-Doping Potentials
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Methyl-, chloro- and fluoro-substitution in the C6 ring has little effect on the oxidation of polybenzothiophene films to the p-doped conducting form, but has a marked effect on reduction to the n-doped form; poly(5,6-dichlorobenzothiophene) is n-do
- King, Geoff,Higgins, Simon J.
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p. 825 - 826
(2007/10/02)
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- THE SYNTHESIS OF 2,3,6,7-TETRASUBSTITUTED NAPHTHALENES: 2,3,6,7-TETRACHLORONAPHTHALENE
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The synthesis of 2,3,6,7-tetrasubstituted naphthalenes and naphthalene derivatives via the cycloaddition reaction of 4,5-dichloro-o-quinodimethane has been accomplished.
- Levy, Louis A.
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p. 639 - 648
(2007/10/02)
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